American Chemical Society
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Synthesis of Taxoids with Improved Cytotoxicity and Solubility for Use in Tumor-Specific Delivery

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journal contribution
posted on 2004-09-23, 00:00 authored by Michael L. Miller, Elizabeth E. Roller, Robert Y. Zhao, Barbara A. Leece, Olga Ab, Erkan Baloglu, Victor S. Goldmacher, Ravi V. J. Chari
To develop effective taxane−antibody immunoconjugates, we have prepared a series of modified taxanes that have both improved toxicity and solubility in aqueous systems as compared to paclitaxel (1a). These taxanes have been modified at either the C-10 or C-7 position and were found to be very cytotoxic against both normal and multi-drug-resistant (MDR) cells, as well as up to 30 times more soluble than paclitaxel in various buffer systems.